Oxaprozin Analogues as Selective RXR Agonists with Superior Properties and Pharmacokinetics

A Novel Co-Crystal of Bexarotene and Ligustrazine Improves Pharmacokinetics and Tissue Distribution of Bexarotene in SD Rats

(2020) Shuyue Ren et al.   Pharmaceutics

Convenient Retinoid X Receptor Binding Assay Based on Fluorescence Change of the Antagonist NEt-C343

(2020) Kayo Yukawa-Takamatsu et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of a “Gatekeeper” Antagonist that Blocks Entry Pathway to Retinoid X Receptors (RXRs) without Allosteric Ligand Inhibition in Permissive RXR Heterodimers

(2020) Masaki Watanabe et al.   JOURNAL OF MEDICINAL CHEMISTRY

Computer-Assisted Discovery and Structural Optimization of a Novel Retinoid X Receptor Agonist Chemotype

(2019) Pascal Heitel et al.   ACS Medicinal Chemistry Letters

Tuning Nuclear Receptor Selectivity of Wy14,643 towards Selective Retinoid X Receptor Modulation

(2019) Julius Pollinger et al.   JOURNAL OF MEDICINAL CHEMISTRY

Unique Polypharmacology Nuclear Receptor Modulator Blocks Inflammatory Signaling Pathways

(2019) Mi Ra Chang et al.   ACS Chemical Biology

3H-Imidazo[4,5-b]pyridine-6-carboxylic Acid Derivatives as Rexinoids with Reduced Teratogenicity

(2019) Yuta Takamura et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Alternative retinoid X receptor (RXR) ligands

(2019) Wojciech Krężel et al.   MOLECULAR AND CELLULAR ENDOCRINOLOGY

Therapeutic modulation of retinoid X receptors – SAR and therapeutic potential of RXR ligands and recent patents

(2019) Simone Schierle et al.   EXPERT OPINION ON THERAPEUTIC PATENTS

Discovery of the First in Vivo Active Inhibitors of the Soluble Epoxide Hydrolase Phosphatase Domain

(2019) Jan S. Kramer et al.   JOURNAL OF MEDICINAL CHEMISTRY

A Novel Biphenyl-based Chemotype of Retinoid X Receptor Ligands Enables Subtype and Heterodimer Preferences

(2019) Julius Pollinger et al.   ACS Medicinal Chemistry Letters

New tools in MolProbity validation: CaBLAM for CryoEM backbone, UnDowser to rethink “waters,” and NGL Viewer to recapture online 3D graphics

(2019) Michael G. Prisant et al.   PROTEIN SCIENCE

Nuclear receptors as potential drug targets in osteoarthritis

(2018) Margaret Man-Ger Sun et al.   CURRENT OPINION IN PHARMACOLOGY

Computer-Assisted Discovery of Retinoid X Receptor Modulating Natural Products and Isofunctional Mimetics

(2018) Daniel Merk et al.   JOURNAL OF MEDICINAL CHEMISTRY

Overview of refinement procedures within REFMAC5: utilizing data from different sources

(2018) Oleg Kovalevskiy et al.   Acta Crystallographica Section D-Structural Biology

Nonacidic Farnesoid X Receptor Modulators

(2017) Daniel Flesch et al.   JOURNAL OF MEDICINAL CHEMISTRY

Tools for ligand validation inCoot

(2017) Paul Emsley   Acta Crystallographica Section D-Structural Biology

Neuronally-directed effects of RXR activation in a mouse model of Alzheimer’s disease

(2017) M. M. Mariani et al.   Scientific Reports

An Endogenous Mammalian Retinoid X Receptor Ligand, At Last!

(2016) Ángel R. de Lera et al.   ChemMedChem

Morphology, in vivo distribution and antitumor activity of bexarotene nanocrystals in lung cancer

(2016) Yongjie Wang et al.   DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY

Phase I/II study of the oral retinoid X receptor agonist bexarotene in Japanese patients with cutaneous T-cell lymphomas

(2016) Toshihisa Hamada et al.   JOURNAL OF DERMATOLOGY

One-pot preparation of 2,5-disubstituted and 2,4,5-trisubstituted oxazoles from aromatic ketones with molecular iodine, oxone, and trifluoromethanesulfonic acid in nitriles

(2015) Sho Imai et al.   TETRAHEDRON

NSAIDs Ibuprofen, Indometacin and Diclofenac do not interact with Farnesoid X Receptor

(2015) Jurema Schmidt et al.   Scientific Reports

Preparation,in vitroandin vivoevaluation of bexarotene nanocrystals with surface modification by folate-chitosan conjugates

(2014) Li Li et al.   DRUG DELIVERY

How good are my data and what is the resolution?

(2013) Philip R. Evans et al.   ACTA CRYSTALLOGRAPHICA SECTION D-BIOLOGICAL CRYSTALLOGRAPHY

Phase I and pharmacokinetic study of bexarotene in combination with gefitinib in the third-line treatment of non-small-cell lung cancer

(2013) Sukhmani K. Padda et al.   ANTI-CANCER DRUGS

Role of bexarotene in the treatment of cutaneous T-cell lymphoma: the clinical and immunological sides

(2013) Alessandro Pileri et al.   Immunotherapy

Defining the Communication between Agonist and Coactivator Binding in the Retinoid X Receptor α Ligand Binding Domain

(2013) LeeAnn J. Boerma et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Therapeutic modulators of peroxisome proliferator-activated receptors (PPAR): a patent review (2008–present)

(2012) Christina Lamers et al.   EXPERT OPINION ON THERAPEUTIC PATENTS

ApoE-Directed Therapeutics Rapidly Clear  -Amyloid and Reverse Deficits in AD Mouse Models

(2012) P. E. Cramer et al.   SCIENCE

Regulation of remyelination in multiple sclerosis

(2011) Khalid A. Hanafy et al.   FEBS LETTERS

XDS

(2010) Wolfgang Kabsch   ACTA CRYSTALLOGRAPHICA SECTION D-BIOLOGICAL CRYSTALLOGRAPHY

Structure, Energetics, and Dynamics of Binding Coactivator Peptide to the Human Retinoid X Receptor α Ligand Binding Domain Complex with 9-cis-Retinoic Acid

(2010) Gang Xia et al.   BIOCHEMISTRY

Retinoid X receptor gamma signaling accelerates CNS remyelination

(2010) Jeffrey K Huang et al.   NATURE NEUROSCIENCE

Bexarotene Induces Dyslipidemia by Increased Very Low-Density Lipoprotein Production and Cholesteryl Ester Transfer Protein-Mediated Reduction of High-Density Lipoprotein

(2009) Jitske de Vries-van der Weij et al.   ENDOCRINOLOGY

Reduction of Lipophilicity at the Lipophilic Domain of RXR Agonists Enables Production of Subtype Preference: RXRα-Preferential Agonist Possessing a Sulfonamide Moiety

(2007) Kayo Takamatsu et al.   ChemMedChem